Preparation and Evaluation of Azelaic Acid Topical Microemulsion Formulation: In Vitro and In Vivo Study

The aim of this study was to design oil in water (O/W) microemulsion formulations for the topical administration of azelaic acid. The permeability of azelaic acid through rat skin and the anti-inflammatory activities of the formulations were conducted to examine the efficacy of the designed formulations. Skin irritation and stability tests were also performed. The permeability of azelaic acid was significantly increased by using O/W microemulsions as carriers. The edema index of ear swelling percentage was significantly recovered by the 5% drug-loaded formulation and a 20% commercial product, demonstrating that the experimental formulation possessed comparable effect with the commercial product on the improvement of inflammation. The experimental formulation did not cause significant skin irritation compared to the negative control group. Moreover, the drug-loaded formulation also showed thermodynamic stability and chemical stability after storage for 30 days. In conclusion, the O/W microemulsion was a potential drug delivery carrier for azelaic acid topical application.

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Combinatory transplantation of mesenchymal stem cells with flavonoid small molecule in acellular nerve graft promotes sciatic nerve regeneration

Journal of Tissue Engineering ◽

10.1177/2041731420980136 ◽

2020 ◽

Vol 11 ◽

pp. 204173142098013

Author(s):

Wen-yuan Li ◽

Hua Jia ◽

Zhen-Dong Wang ◽

Feng-guo Zhai ◽

Guang-da Sun ◽

...

Keyword(s):

Spinal Cord ◽

Cell Differentiation ◽

Small Molecule ◽

Negative Control Group ◽

Negative Control ◽

Nerve Graft ◽

Lumbar Spinal Cord ◽

Control Group

Previous animal studies have demonstrated that the flavonoid small-molecule TrkB agonist, 7, 8-dihydroxyflavone (DHF), promotes axon regeneration in transected peripheral nerves. In the present study, we investigated the combined effects of 7, 8-DHF treatment and bone marrow-derived stem/stromal cells (BMSCs) engraftment into acellular nerve allografts (ANAs) and explore relevant mechanisms that may be involved. Our results show that TrkB and downstream ERK1/2 phosphorylation are increased upon 7, 8-DHF treatment compared to the negative control group. Also, 7, 8-DHF promotes proliferation, survival, and Schwann-like cell differentiation of BMSCs in vitro. While selective ERK1/2 inhibitor U0126 suppressed the effect of upregulation of ERK1/2 phosphorylation and decreased cell proliferation, survival, and Schwann-like cell differentiation partially induced by 7, 8-DHF. In vivo, 7, 8-DHF promotes survival of transplanted BMSCs and upregulates axonal growth and myelination in regenerating ANAs. 7, 8-DHF+BMSCs also improved motor endplate density of target musculature. These benefits were associated with increased motor functional recovery. 7, 8-DHF+BMSCs significantly upregulated TrkB and ERK1/2 phosphorylation expression in regenerating ANA, and increased TrkB expression in the lumbar spinal cord. The mechanism of 7, 8-DHF action may be related to its ability to upregulate TrkB signaling, and downstream activation of survival signaling molecules ERK1/2 in the regenerating ANAs and spinal cord and improved survival of transplanted BMSCs. This study provides novel foundational data connecting the benefits of 7, 8-DHF treatment in neural injury and repair to BMSCs biology and function and demonstrates a potential combination approach for the treatment of injured peripheral nerve via nerve graft transplant.

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Celery (Apium graveolens) as a potential antibacterial agent and its effect on cytokeratin-17 and other healing promoters in skin wounds infected with methicillin-resistant Staphylococcus aureus

Veterinary World ◽

10.14202/vetworld.2020.865-871 ◽

2020 ◽

Vol 13 (5) ◽

pp. 865-871

Author(s):

Yos Adi Prakoso ◽

Chylen Setiyo Rini ◽

Asih Rahayu ◽

Miarsono Sigit ◽

Dyah Widhowati

Keyword(s):

Staphylococcus Aureus ◽

Bacterial Colonization ◽

Negative Control Group ◽

Negative Control ◽

Apium Graveolens ◽

Control Group ◽

Sprague Dawley ◽

Methicillin Resistant

Background and Aim: Antimicrobial resistance is a global problem caused by extensive utilization of antibiotics that promote gene resistant among bacteria, including Staphylococcus aureus. This study aimed to analyze the potential effects of celery (Apium graveolens) extract as an antioxidant and antimicrobial agent against methicillin-resistant S. aureus (MRSA), in vitro and in vivo. Materials and Methods: Celery was extracted and tested against a MRSA isolate in vitro. The minimum inhibitory concentration (MIC) against MRSA for the celery extract (CE) was determined to be 0.1% and it was formulated into a cream. A total of 30 female Sprague Dawley rats were divided into five groups: Group 1, negative control; Group 2, positive control; Group 3, treated with 0.05% CE cream; Group 4, 0.1% CE cream; and Group 5, 0.2% CE cream. All animals in the groups were exposed to a full-thickness skin biopsy on the dorsal portion, and they were infected with 30 μL of 105 colony-forming units of the MRSA isolate. The treatment was administered twice a day for 7 days. The skin samples were collected on days 3 and 7 after the treatment. The skin tissue was examined histologically using hematoxylin and eosin, Gram staining, and immunohistochemistry against cytokeratin (CK)-17. Results: Results showed that 0.2% of CE cream was the best treatment for wounds infected with MRSA. CE (0.2%) cream increased skin reepithelialization, fibroblast proliferation, and CK-17 expression; it also decreased the percentage of wound area, inflammatory cell infiltration, and bacterial colonization in skin wound tissue compared to the other treatments (p≤0.05). Conclusion: This study demonstrated that celery could be utilized as an alternative herbal therapy against MRSA-associated skin infections.

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Enhancement of the Topical Bioavailability and Skin Whitening Effect of Genistein by Using Microemulsions as Drug Delivery Carriers

Pharmaceuticals ◽

10.3390/ph14121233 ◽

2021 ◽

Vol 14 (12) ◽

pp. 1233

Author(s):

Quoc Lam Vu ◽

Chih-Wun Fang ◽

Muhammad Suhail ◽

Pao-Chu Wu

Keyword(s):

Drug Delivery ◽

Skin Irritation ◽

Topical Administration ◽

Skin Whitening ◽

Drug Delivery Carrier ◽

In Vitro Permeation ◽

Topical Bioavailability ◽

The Mean

Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induced skin carcinogenesis in hairless mice and UVB-induced erythema on human skin. In current study, genistein-loaded microemulsions were developed by using the various compositions of oil, surfactants, and co-surfactants and used as a drug delivery carrier to improve the solubility, peremability, skin whitening, and bioavailbility of genistein. The mean droplet size and polydispersity index of all formulations was less than 100 nm and 0.26 and demonstrated the formation of microemulsions. Similarly, various studies, such as permeation, drug skin deposition, pharmacokinetics, skin whitening test, skin irritation, and stability, were also conducted. The permeability of genistein was significantly affected by the composition of microemulsion formulation, particular surfactnat, and cosurfactant. In-vitro permeation study revealed that both permeation rate and deposition amount in skin were significantly increased from 0.27 μg/cm2·h up to 20.00 μg/cm2·h and 4.90 up to 53.52 μg/cm2, respectively. In in-vivo whitening test, the change in luminosity index (ΔL*), tended to decrease after topical application of genistein-loaded microemulsion. The bioavailability was increased 10-fold by topical administration of drug-loaded microemulsion. Conclusively, the prepared microemulsion has been enhanced the bioavailability of genistein and could be used for clinical purposes.

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Effectiveness of Frangipani Leaf Extract (Plumeria alba Linn.) as a UV Filter

BERITA BIOLOGI ◽

10.14203/beritabiologi.v20i2.3951 ◽

2021 ◽

Vol 20 (2) ◽

pp. 191-200

Author(s):

Irein Kusuma Angreini ◽

Aniek Prasetyaningsih ◽

Vinsa Cantya Prakasita

Keyword(s):

Crude Extract ◽

Clinical Symptoms ◽

Pearson Correlation ◽

Negative Control Group ◽

Negative Control ◽

Control Group ◽

Uv Filters ◽

Uv Filter

UV filters are necessary since UV rays are harmful to human skin. UV filter compounds in commercial sunscreen products can cause adverse effects. Thus, natural UV filters containing flavonoids, e.g. Frangipani (Plumeria alba Linn.) leaves, are needed. This research examined the use of flavonoids from P. alba leaf as a UV filter with in vitro and in vivo. Maceration was performed with 70% ethyl alco-hol and liquid-liquid extraction for flavonoid purification. Parameters tested were total flavonoid compounds, SPF value, and clinical symptoms of the melanogenesis inhibition scoring. The purification result was 43.6%. The flavonoid concentration in pure extract (64.4 mg QE /g) was higher than crude extract (57.6 mg QE/g). The highest SPF value (33.88) was observed in pure extract at 1400 mg/mL, while the same concentration of crude extract resulted in a lower SPF value (33.06). Pearson correlation analysis (0.536) indicated a di-rectly proportional relationship between SPF value and extract concentration. In vivo analysis was performed by scoring between 0-4 following the severity of erythema. After 21 days of sunlight exposure, the worst erythema was found in the negative control group (score 1.292). The best result was found in the group treated with pure extract 1400 mg/ml (score 0.542).

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Improved percutaneous delivery of azelaic acid employing microemulsion as nanocarrier: formulation optimization, in vitro and in vivo evaluation

RSC Advances ◽

10.1039/c5ra00713e ◽

2015 ◽

Vol 5 (37) ◽

pp. 28985-28995 ◽

Cited By ~ 6

Author(s):

Huixian Ma ◽

Meng Yu ◽

Fengping Tan ◽

Nan Li

Keyword(s):

Azelaic Acid ◽

Skin Irritation ◽

Topical Administration ◽

In Vivo Evaluation ◽

Formulation Optimization

Topical administration of an optimal microemulsion could effectively enhance the amount of azelaic acid in skin without causing skin irritation.

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Genotoxic and Chemopreventive Effects of Vochysia divergens Leaves (Pantanal, Brazil)

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2018/6596142 ◽

2018 ◽

Vol 2018 ◽

pp. 1-7

Author(s):

Pollyanna Francielli de Oliveira ◽

Suzana Amorim Mendes ◽

Nathália Oliveira Acésio ◽

Luis Claudio Kellner Filho ◽

Leticia Pereira Pimenta ◽

...

Keyword(s):

Protective Effect ◽

Skin Diseases ◽

Chemical Constituents ◽

Test System ◽

Negative Control ◽

Control Group ◽

Xtt Assay ◽

Vochysia Divergens

The medicinal plant Vochysia divergens is a colonizing tree species of the Pantanal, a unique and little explored wetland region in Brazil. This species is used in folk medicine as syrups and teas to treat respiratory infections, digestive disorders, asthma, scarring, and skin diseases. The objectives of this study were to evaluate the antioxidant, cytotoxic, and genotoxic potential of the ethanolic extract of Vochysia divergens leaves (VdE), as well as the influence of VdE and its major component (the flavone 3′,5-dimethoxy luteolin-7-O-β-glucopyranoside; 3′5 DL) on MMS-induced genotoxicity. The extract significantly reduced the viability of V79 cells in the colorimetric XTT assay at concentrations ≥ 39 μg/mL. A significant increase in micronucleus frequencies was observed in V79 cell cultures treated with VdE concentrations of 160 and 320 μg/mL. However, animals treated with the tested doses of VdE (500, 1000, and 2000 mg/kg b.w.) exhibited frequencies that did not differ significantly from those of the negative control group, indicating the absence of genotoxicity. The results also showed that VdE was effective in reducing MMS-induced genotoxicity at concentrations of 20, 40, and 80 μg/mL in the in vitro test system and at a dose of 15 mg/kg b.w. in the in vivo test system. Its major component 3′5 DL exerted no protective effect, suggesting that it is not responsible for the effect of the extract. The results of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay showed that VdE was able to scavenge 92.6% of free radicals. In conclusion, the results suggest that the protective effect of VdE may be related, at least in part, to the antioxidant activity of its chemical constituents.

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In vitro comparison of the cytotoxicity of different endodontic sealers; AH Plus, AdSeal, Endoseal MTA, and GuttaFlow Bioseal

10.21203/rs.3.rs-1017752/v1 ◽

2021 ◽

Author(s):

Mehdi Dastorani ◽

Muhammad javad Aliee ◽

Raheleh Halabian ◽

Mostafa Solati ◽

Mohammadsadegh Alemrajabi

Keyword(s):

Repeated Measures ◽

Negative Control Group ◽

Negative Control ◽

Control Group ◽

Gingival Fibroblasts ◽

Periapical Lesions ◽

Ah Plus ◽

Low Cytotoxicity ◽

Endodontic Sealers

Abstract Background: This study aimed to assess the cytotoxicity of four commonly used endodontic sealers namely AH Plus, AdSeal, Endoseal MTA, and GuttaFlow Bioseal against human gingival fibroblasts (HGFs). Methods: After culturing the HGFs, they were exposed to the respective sealers in set form and in five different weights, after sterilization. The cytotoxicity of the sealers was evaluated after 1, 3 and 7 days using the methyl thiazolyl tetrazolium (MTT) assay. Data were analyzed by repeated measures ANOVA. Results: After 24 h, all sealers showed low cytotoxicity. However, all sealers in 250 mg and 500 mg weights showed significantly higher cytotoxicity than the negative control group at 72 h, and 7 days (P<0.05) except for AdSeal in 80 mg weight (P>0.05). AH Plus was significantly more cytotoxic than other sealers at 3 and 7 days (P<0.05) while AdSeal had the closest results to the negative control group, and showed significantly higher biocompatibility than other sealers in 250 mg concentration. Conclusion: AdSeal showed the highest biocompatibility while AH Plus had the highest cytotoxicity among the tested sealers. Thus, its application may delay the healing of periapical lesions.

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Antiproliferation Effects of Nanophytosome-Loaded Phenolic Compounds From Fruit of Juniperus Polycarpos Against Breast Cancer in Mice Model: Synthesis, Characterization and Therapeutic Effects

10.21203/rs.3.rs-1073994/v1 ◽

2021 ◽

Author(s):

Soheila Moeini ◽

Ehsan Karimi ◽

Ehsan Oskoueian

Keyword(s):

Breast Cancer ◽

Negative Control Group ◽

Negative Control ◽

Control Group ◽

Therapeutic Effects ◽

Mice Model ◽

Fruit Extract ◽

Phenolic Fraction ◽

Juniperus Polycarpos

Abstract Background: This research was performed to synthesize nanophytosomes-loaded high phenolic fraction (HPF) from Juniperus polycarpos fruit extract and investigate its antiproliferation effects against breast cancer in mice model. Results: The nanophytosomes-loaded HPF from Juniperus polycarpos fruit extract was synthesized. The mice trial was conducted to determine the possible toxic effects of the synthesized nanophytosomes. The anticancer, pro-apoptotic, and antioxidative activities of the nanophytosomes were determined. The nanophytosomes-loaded HPF had a spherical structure with a size of 176 nm and a polydispersity index coefficient of 0.24. The in-vivo study manifested that nanophytosomes-loaded HPF significantly improved weight gain and food intake compared to the negative control group (p<0.05). The nanophytosomes-loaded HPF significantly enhanced the expression of bax (3.4-fold) and caspase-3 (2.7-fold) genes but reduced bcl2 (3.6-fold) gene expression in tumor cells. The average tumor size was significantly decreased in mice treated with nanophytosomes-loaded HPF (p<0.05). The expression of GPX (2.3-fold) and SOD (2.7-fold) antioxidants in the liver of mice supplemented with nanophytosomes-loaded HPF was significantly developed compared to the negative control (p<0.05). The nanophytosomes-loaded HPF did not show toxicity on normal cells. Conclusion: Our results indicated that nanophytosomes-loaded HPF might be a potential anticancer agent for the breast cancer treatment.

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THE PROTECTIVE ROLE OF OMEGA-3 AGAINST GENOTOXICITY AND REPRODUCTIVE TOXICITY OF COBALT OXIDE NANOPARTICLES ACUTE TREATMENT IN MALE MICE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i5.25245 ◽

2018 ◽

Vol 11 (5) ◽

pp. 423

Author(s):

Nahed A Hussien ◽

Hanan R. H. Mohamed

Keyword(s):

Cobalt Oxide ◽

Negative Control Group ◽

Protective Role ◽

Negative Control ◽

Control Group ◽

Omega 3 ◽

Genotoxic Potential ◽

Polychromatic Erythrocytes

Objective: Cobalt nanoparticles (NPs), especially cobalt oxide NPs (Co3O4 NPs) are attracting unique shaped NPs that are used in different biomedical applications and medicine. Different in vitro studies report their toxic and carcinogenic effect but limited in vivo studies were present on its genotoxic potential. The present study was aimed to evaluate the genotoxic potential of Co3O4 NPs on bone marrow cells and sperms and the protective role of omega-3 in male albino mice.Methods: Animals were segregated into four groups that were orally treated for 3 consecutive days, Group 1: Negative control; Group 2: Omega-3 (250 mg/kg); Group 3: Co3O4 NPs (20 mg/kg); and Group 4: Combined group (250 mg/kg Omega-3 and Co3O4 NPs 20 mg/kg).Results: The present results show that Co3O4 NPs administration significantly increased number of micronucleated polychromatic erythrocytes (PCEs)/1000 PCEs, sperm abnormalities, and DNA damage, significantly decreased sperm motility and concentration in comparison to negative control group. However, Omega-3 administration in the combined group modulates the genotoxic potential of Co3O4 NPs in comparison to Co3O4 NPs group.Conclusion: The present study reports the genotoxic potential of Co3O4 NPs in vivo and assesses the protective role of Omega-3 administration due to its antioxidant effect.

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Antibacterial Activity of Curcuma longa (turmeric), Curcuma zedoaria (zedoary), and Allium sativum (garlic) Nanoparticle Extract on Chicken with Chronic Respiratory Disease Complex: In Vivo Study

E3S Web of Conferences ◽

10.1051/e3sconf/202015101054 ◽

2020 ◽

Vol 151 ◽

pp. 01054

Author(s):

Ekowati Handharyani ◽

Lina N. Sutardi ◽

Aulia A. Mustika ◽

Andriani Andriani ◽

Sri Yuliani

Keyword(s):

Antibacterial Activity ◽

Respiratory Disease ◽

Allium Sativum ◽

Curcuma Longa ◽

Clinical Signs ◽

Chronic Respiratory Disease ◽

Negative Control ◽

Control Group

Previous in vitro studies showed that nanoparticle extract of turmeric, zedoary, and garlic exhibit antibacterial activity against Mycoplasma gallisepticum (M. gallisepticum) which causes chronic respiratory disease (CRD) in chicken. This research aimed to determine the antibacterial activity of nanoparticles of Curcuma longa, Curcuma zedoaria, and Allium sativum extract to CRD infected chicken. In vivo test of antibacterial activity of turmeric, zedoary, and garlic nanoparticle in combination was conducted on chicken infected by M. gallisepticum and Escherichia coli (E.coli). Antibiotic control used was enrofloxacin. As many as 75 chickens were divided into 5 groups containing 15 chickens each. Group one consisted of healthy chickens (positive control); group two consisted of chickens that have been inoculated by bacteria (negative control); group three (treatment) were chickens inoculated by bacterium and given extract nanoparticle combination on day 7 of infection for 7 days; group four (prevention) were chickens inoculated by bacterium and given combination of extract nanoparticles on day 5 before infection for 14 days; group five were chickens inoculated with bacterium and given enrofloxacin antibiotics for 7 days. In vivo research results showed increased body weight and performance indicated by improvements in clinical signs, and gross pathology changes. The combination of three extract nanoparticles showed the best activity in controlling CRD in chicken, both as preventive and curative means.

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